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Donepezil plus chromone plus melatonin hybrids as promising agents for Alzheimer's disease therapy

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dc.contributor.authorPachon-Angona, Irene
dc.contributor.authorRefouvelet, Bernard
dc.contributor.authorAndrýs, Rudolf
dc.contributor.authorMartin, Helene
dc.contributor.authorLuzet, Vincent
dc.contributor.authorIriepa, Isabel
dc.contributor.authorMoraleda, Ignacio
dc.contributor.authorDiez-Iriepa, Daniel
dc.contributor.authorOset-Gasque, Maria-Jesus
dc.contributor.authorMarco-Contelles, Jose
dc.contributor.authorMusílek, Kamil
dc.contributor.authorIsmaili, Lhassane
dc.date.accessioned2026-08-18T12:31:23Z
dc.date.issued2019
dc.description.abstractWe describe herein the design, multicomponent synthesis and biological studies of new donepezil + chromone + melatonin hybrids as potential agents for Alzheimer's disease (AD) therapy. We have identified compound 14n as promising multitarget small molecule showing strong BuChE inhibition (IC50 = 11.90 +/- 0.05 nM), moderate hAChE (IC50 = 1.73 +/- 0.34 mu M), hMAO A (IC50 = 2.78 +/- 0.12 mu M), and MAO B (IC50 = 21.29 +/- 3.85 mu M) inhibition, while keeping a strong antioxidant power (3.04 TE, ORAC test). Consequently, the results reported here support the development of new multitarget Donepezil + Chromone + Melatonin hybrids, such as compound 14n, as a potential drug for AD patients cure.eng
dc.description.abstract-translatedWe describe herein the design, multicomponent synthesis and biological studies of new donepezil + chromone + melatonin hybrids as potential agents for Alzheimer's disease (AD) therapy. We have identified compound 14n as promising multitarget small molecule showing strong BuChE inhibition (IC50 = 11.90 +/- 0.05 nM), moderate hAChE (IC50 = 1.73 +/- 0.34 mu M), hMAO A (IC50 = 2.78 +/- 0.12 mu M), and MAO B (IC50 = 21.29 +/- 3.85 mu M) inhibition, while keeping a strong antioxidant power (3.04 TE, ORAC test). Consequently, the results reported here support the development of new multitarget Donepezil + Chromone + Melatonin hybrids, such as compound 14n, as a potential drug for AD patients cure.cze
dc.formatp. 479-489
dc.identifier.doi10.1080/14756366.2018.1545766
dc.identifier.issn1475-6366
dc.identifier.obd43875031
dc.identifier.scopus2-s2.0-85061054004
dc.identifier.urihttps://hdl.handle.net/20.500.12603/3129
dc.identifier.wos000457532600001
dc.language.isoeng
dc.peerreviewedyes
dc.project.IDIRP 1902/2018
dc.publicationstatuspostprint
dc.publisherTaylor & Francis
dc.relation.ispartofJournal of enzyme inhibition and medicinal chemistry, volume 34, issue: 1eng
dc.relation.publisherversionhttps://www.tandfonline.com/doi/full/10.1080/14756366.2018.1545766
dc.rights.accessOpen Access
dc.rights.licenseCC BY
dc.source.urlhttps://www.tandfonline.com/doi/full/10.1080/14756366.2018.1545766
dc.subjectAntioxidanteng
dc.subjectcholinesteraseseng
dc.subjectdonepezileng
dc.subjectMAO-Aeng
dc.subjectMAO-Beng
dc.subjectORACeng
dc.subjectUgi-4MCReng
dc.subjectAntioxidantcze
dc.subjectcholinesterasescze
dc.subjectdonepezilcze
dc.subjectMAO-Acze
dc.subjectMAO-Bcze
dc.subjectORACcze
dc.subjectUgi-4MCRcze
dc.titleDonepezil plus chromone plus melatonin hybrids as promising agents for Alzheimer's disease therapyeng
dc.title.alternativeDonepezil plus chromone plus melatonin hybrids as promising agents for Alzheimer's disease therapycze
dc.typearticle

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